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Papers of the Week

2021 May 10

Trends Pharmacol Sci

Structural insights into ligand recognition and activation of angiotensin receptors.


Zhang H, Luginina A, Mishin A, Baidya M, Shukla AK, Cherezov V
Trends Pharmacol Sci. 2021 May 10.
PMID: 33985815.


G protein-coupled angiotensin II receptors, ATR and ATR, are integral components of the renin-angiotensin system (RAS) that regulates blood pressure and fluid balance in humans. While ATR is a well-established target of angiotensin receptor blockers (ARBs) for managing hypertension and a prime system for studying biased signaling, ATR has been recognized as a promising target against neuropathic pain and lung fibrosis. In this review, we discuss how recent structural advances illuminate ligand-binding modes and subtype selectivity, shared and distinct features of the receptors, their transducer-coupling patterns, and downstream signaling responses. We also underscore the key ATR aspects that require further studies to fully appreciate the mechanistic framework that fine-tunes their cellular and physiological functions, providing untapped potential for drug discovery.